2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl → N-(2,5-Difluoro-4-(morpholinomethyl)phenyl)-5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine hydrochloride

Participants

Reaction Conditions

Reaction Steps

5-Fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine (432 mg, 1.56 mmol) was dissolved in 1,4-dioxane (18 ml) and 4-(4-chloro-2,5-difluorobenzyl)morpholine (390 mg, 1.57 mmol) and potassium tert-butoxide (230 mg, 2.05 mmol) were added. The mixture was flushed with argon and stirred for 5-10 minutes. Tris(dibenzylideneacetone)dipalladium(0) (144 mg, 0.16 mmol) and 2-dicyclohexylphosphino-2′,4′,6′-tri-iso-propyl-1,1′-biphenyl (150 mg, 0.31 mmol) were added. The mixture was heated at 102° C. under an atmosphere of argon for 3 h.

Provenance & Evidence